AG-012986
Product Specifications
CAS Number
486414-35-1
Target
Others|||CDK
Related Pathways
Others|||Cell Cycle/Checkpoint
Bioactivity
AG-012986 is a multitargeted cyclin-dependent kinase (CDK) inhibitor active against CDK1, CDK2, CDK4/6, CDK5, and CDK9, with selectivity over a diverse panel of non-CDK kinases. AG-012986 showed antiproliferative activities in vitro with IC (50) s of <100 nmol/L in 14 of 18 tumor cell lines. In vivo, significant antitumor efficacy induced by AG-012986 was seen (tumor growth inhibition, >83.1%) in 10 of 11 human xenograft tumor models. AG-012986 also showed dose-dependent retinoblastoma Ser (795) hypophosphorylation, cell cycle arrest, decreased Ki-67 tumor staining, and apoptosis in conjunction with antitumor activity.
Smiles
C(=O)(C=1SC(NC2=CC=C(C(N[C@@H](CN(C)C)C)=O)C=C2)=NC1N)C3=C(F)C=CC=C3F
Molecular Formula
C22H23F2N5O2S
Molecular Weight
459.51
Shipping Conditions
Cool pack
Storage Temperature
-20°C
Available Sizes
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